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Assay Detail

CHEMBL840422

Review assay metadata, readout intent, target linkage, and publication context from the same page.

Functional
In vitro inhibition of ET-1 stimulated vasoconstriction in rabbit femoral artery.
4
Total Activities
4
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Oryctolagus cuniculus
Tissue Femoral artery
Confidence 4 — Cell-line / Tissue
Curated By Autocuration

Target

Endothelin receptor, ET-A/ET-B (CHEMBL2096678)
Type PROTEIN FAMILY
Organism Homo sapiens

Publication

1-benzyl-3-thioaryl-2-carboxyindoles as potent non-peptide endothelin antagonists
Bunker AM, Edmunds JJ, Berryman KA, Walker DM, Flynn MA, Welch KM, Doherty AM
Bioorg Med Chem Lett (1996) 6 : 1367 -1370
· DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Kd 4 7.00 7.50

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL287169 1 7.50
CHEMBL27732 1 7.30
CHEMBL28920 1 6.90
CHEMBL28563 1 6.30

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL287169 Kd = 31.62 nM 7.50
CHEMBL27732 Kd = 50.12 nM 7.30
CHEMBL28920 Kd = 125.89 nM 6.90
CHEMBL28563 Kd = 501.19 nM 6.30